Analysis of the differences between pemetinib (Dabotan) and first-, second- and third-generation targeted drugs

Pemigatinib is an oral small molecule FGFR (fibroblast growth factor receptor) inhibitor, mainly used to treat cholangiocarcinoma and other related tumors with FGFR2 gene fusion or rearrangement. Compared with traditional first-generation targeted drugs, pemetinib has significantly improved selectivity and targeting accuracy, and can specifically inhibit the FGFR signaling pathway, thereby reducing the inhibitory effect on non-targets and related toxic and side effects.

Compared with first-generation targeted drugs, second- and third-generation targeted drugs usually have improved coverage of drug-resistant mutations and drug affinity. Most of the first-generation targeted drugs are broad-spectrum tyrosine kinase inhibitors, which are prone to drug resistance and have relatively obvious side effects. As a new generation FGFR inhibitor, pemetinib has better inhibitory ability in the face of drug-resistant mutations, can delay disease progression and improve the clinical benefit period of patients.

The third generation of targeted drugs has been further improved in terms of structure optimization and pharmacokinetics, and can overcome some specific mutation resistance mechanisms. In contrast, pemetinib's design emphasizes the precise inhibition of FGFR2fusion / rearrangement. It also performs better in terms of safety and tolerability, allowing patients to control side effects during long-term treatment and making treatment management more convenient.

In general, the advantages of pemetinib lie in its high targeting accuracy, relatively wide coverage of drug-resistant mutations, and its advantages over early targeted drugs in managing toxic and side effects. Clinically, pemetinib can be used as a first-line or follow-up treatment option for patients with specific gene mutations, providing a more precise treatment strategy for cholangiocarcinoma and related diseases.

Keyword tags:

Pemetinib, FGFR inhibitor, cholangiocarcinoma, generation of targeted drugs, precise targeting, drug-resistant mutations, safety

Reference materials:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8170298/